1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. Sodium Channel
    TRP Channel
  3. Phenamil methanesulfonate

Phenamil methanesulfonate 

Cat. No.: HY-108464A
Handling Instructions

Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM. Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca2+ transport with an IC50 of 140 nM in a Ca2+ uptake assay. Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease.

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Phenamil methanesulfonate Chemical Structure

Phenamil methanesulfonate Chemical Structure

CAS No. : 1161-94-0

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Description

Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM[2]. Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca2+ transport with an IC50 of 140 nM in a Ca2+ uptake assay[1]. Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway[4]. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease[5].

IC50 & Target[1]

TRPC3

140 nM (IC50)

In Vitro

TRPP3, a member of the transient receptor potential (TRP) superfamily of cation channels, is a Ca2+-activated channel permeable to Ca2+, Na+, and K+. TRPP3 is implicated in regulation of pH-sensitive action potential in spinal cord neurons.
Phenamil methanesulfonate (1 μM) decreases 45Ca2+ uptake in a radiotracer uptake assay. It inhibits TRPP3-mediated Ca2+ transport with an IC50 value of 0.28 μM in oocytes expressing TRPP3 or H2O-injected oocytes[1].
Phenamil methanesulfonate is a more potent ENaC blocker than Amiloride, it inhibits the epithelial sodium channel (ENaC) with an IC50 of 400 nM (Amiloride=776 nM)[2].
Phenamil methanesulfonate inhibits basal short-circuit currents with IC50 values of 75 and 116 nM, respectively in both human and ovine bronchial epithelia cells[3].
Phenamil methanesulfonate (0-20 μM; 14 days) elevates adipogenic gene expression, PPARγ, Fabp4, and lipoprotein lipase expression in a concentration-dependent manner ,and regulates adipogenesis in C3H10T1/2 cells[4].
Phenamil methanesulfonate (0-20 μM; 7 or 14 days) modulates MC3T3-E1 osteoblastic differentiation, it increases Alkaline phosphatase (ALP) activity in MC3T3-E1 cells in a concentration-dependent manner[4].

RT-PCR[4]

Cell Line: C3H10T1/2 cells
Concentration: 0 μM and 20 μM
Incubation Time: 14 days
Result: Increased PPARγ, Fabp4, and lipoprotein lipase (LPL) mRNA expression.
In Vivo

Phenamil methanesulfonate (subcutaneous injection; 15 or 30 mg/kg; 21 days; infusion rate of 1 ml/h) reduces chronic-hypoxia-induced pulmonary artery hypertension (PAH). Additionally, the mRNA level of SMA, SM22, Id3, and Trb3 from the lung sample are also decreased by Phenamil under hypoxia or normoxia in rats. However, phenamil has little effect on pulmonary vasculature under physiological conditions[5].

Animal Model: Male Sprague-Dawley rats[5]
Dosage: 15 or 30 mg/kg
Administration: Subcutaneous injection; 15 or 30 mg/kg; 21 days; infusion rate of 1 ml/h
Result: Reduced hypoxia-induced pulmonary hypertension and vascular remodeling. 
Molecular Weight

401.83

Formula

C₁₃H₁₆ClN₇O₄S

CAS No.

1161-94-0

SMILES

O=C(C1=NC(Cl)=C(N)N=C1N)NC(NC2=CC=CC=C2)=N.CS(=O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PhenamilSodium ChannelTRP ChannelNa channelsNa+ channelsTransient receptor potential channelsOBE CellsCystic FibrosisLung DiseaseENaCmucus clearanceMCCFairwaysMC3T3-E1osteoblasticdifferentiationPulmonaryarteryhypertensionPAHInhibitorinhibitorinhibit

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Phenamil methanesulfonate
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